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Classical Alkylating Agents: Mustardgen

The document discusses various classes of classical alkylating agents used in chemotherapy. It lists the main groups - nitrogen mustards, nitrosoureas, and alkyl sulfonates. Examples of agents from each group are provided. Platinum-based drugs that act similar to alkylating agents through DNA damage are also discussed.

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DR Salih Ibrahim
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74 views

Classical Alkylating Agents: Mustardgen

The document discusses various classes of classical alkylating agents used in chemotherapy. It lists the main groups - nitrogen mustards, nitrosoureas, and alkyl sulfonates. Examples of agents from each group are provided. Platinum-based drugs that act similar to alkylating agents through DNA damage are also discussed.

Uploaded by

DR Salih Ibrahim
Copyright
© Attribution Non-Commercial (BY-NC)
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as DOCX, PDF, TXT or read online on Scribd
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Classical alkylating agents

Many of the agents are known as "Classical alkylating agents". These include true alkyl groups, and have been known for a longer time than some of the other alkylating agents. Examples include melphalan and chlorambucil. The following three groups are almost always considered "classical".

Nitrogen mustards Cyclophosphamide Mechlorethamine or mustine (HN2) (trade name Mustardgen) Uramustine or uracil mustard Melphalan Chlorambucil Ifosfamide

Nitrosoureas

Carmustine Lomustine Streptozocin

Alkyl sulfonates

Busulfan

Thiotepa and its analogues are usually considered classical, but can be considered nonclassical.

Alkylating-like
Platinum-based chemotherapeutic drugs (termed platinum analogues) act in a similar manner. These agents do not have an alkyl group, but nevertheless damage DNA They permanently coordinate to DNA to interfere with DNA repair, so they are sometimes described as "alkylatinglike".

Platinum (2) Cisplatin (3)Carboplatin (4)Nedaplatin (5) Oxaliplatin (6)Satraplatin (7)Triplatin tetranitrate

These agents also bind at N7 of guanine.


Antitumor drugs can be classified according to their effect on the mitotic cycle:

1. Cell cycle active, phase specific 2. Cell cycle active, non-phase specific 3. Non-cell cycle active Following are some of the various classes of chemotherapy drugs based on their chemical structure and the mechanism they use to attack cancer cells: Alkylating Agents Alkylating agents are the oldest and most commonly used class of chemotherapy drugs, and work by directly damaging DNA and preventing cancer cells from reproducing. They are used to treat a wide variety of cancers, but have the greatest effect on those that are slow-growing. They are cell-cycle phase non-specific, meaning that they kill cancer cells in any phase of the cell cycle. Some examples of alkylating agents are carboplatin, cisplatin and oxaliplatin. Antimetabolites Antimetabolites are chemotherapy drugs that interfere with DNA and RNA growth. They are cell-cycle specific, meaning that they kill cancer cells in a specific phase of cell division. Some examples of antimetabolites are capecitabine, gemcitabine, and pemetrexed (Alimta). Anthracyclines Anthracyclines are anti-tumor antibiotics that interfere with enzymes necessary for DNA replication. They are cell-cycle non-specific, and are used to treat a variety of cancers. Some examples of anthracyclines are bleomycin, doxorubicin and mitomycin-C. Plant Alkaloids Plant alkaloids are derived from certain types of plants found in nature, and inhibit or prevent mitosis or inhibit enzymes from making proteins necessary for cell reproduction. Most plant alkaloids are cell-cycle specific, but can cause damage in all phases. Some examples of plant alkaloids are the taxanes, docetaxel and paclitaxel, and the vinca alkaloids, vinblastine, vincristine and vinorelbine. All of these have been employed in the treatment of mesothelioma at some time. More on non-phasespecific chemotherapy agents.

Alkylating Agents
It interferes with rapidly reproducing cell DNA; indicated for cancer of the blood (leukemia).

Examples: Busulfan (Myleran), Chlorambucil (Leukeran), Cisplatin platinol- AQ, Cyclophosphamide (Cytoxan)

Antimetabolites
Counterfeits cell division of cancer cells thus preventing metastatic growth; indicated for cancer in the colon, breast, stomach and pancreas Examples: Cytarabine (ARA-C), Flourouracil (5-FL), Hydroxyurea (Hydrea), Mercaptopurine (6-MP), Methotrexate (MTX)

Antitumor Agents
It acts primarily by interfering DNA and RNA synthesis preventing rapid cancer cell growth; indicated for several types of cancer. Examples: Bleomycin ( Blenoxane), Dactinomycin (Actinomycin D), Doxorubicin (Adriamycin)

Hormonal Agents
Changes hormone input into sensitive agents; primarily indicated for breast cancer Examples: Tamoxifen, testosterone

Vinca Alkaloids
Plant alkaloids that act as mitotic inhibitor and interferes with cell division; indicated primarily for lymphoma, cancers, hodgkins disease Examples: Vinblastine(Velban), Vincristine (Oncovin)

Topoismerase
Drugs that bind to enzyme that breaks the DNA strands thus, preventing cancer cells formation and metastasis; indicated for airway, lung, colon, and rectal cancers. Examples: Irinotecan (Camptosar), Topotecan (Hycamtin)

Steroids
Reduce edema and inflammation around a tumor and useful for symptom relief; indicated for several types of cancer. Examples: Androgen, Estrogen, Progestin

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